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Alternate Method for the Synthesis of Six-Membered Carbocycles with Five Stereocenters: 1,2,3,4,6-Pentasubstituted-4-hydroxy-cyclohexanes
(TAYLOR & FRANCIS INC, 2015) Gezegen, Hayreddin; Ceylan, Mustafa
A series of novel 1,2,3,4,6-pentasubstituted-4-hydroxy-cyclohexanes (3a-u) were synthesized from the reaction of aromatic ketones with aromatic aldehydes under mild reaction conditions in good yields. The stereochemistry of the synthesized compounds was established using 1D and 2D-NMR spectra.
Antiproliferative Evaluation of Some 2-[2-(2-Phenylethenyl)-cyclopent-3-en-1-yl]-1,3-benzothiazoles: DFT and Molecular Docking Study
(Wiley-V C H Verlag Gmbh, 2020) Ceylan, Mustafa; Erkan, Sultan; Yaglioglu, Ayse Sahin; Uremis, Nuray Akdogan; Koc, Esra
The 2-[2-(2-phenylethenyl)cyclopent-3-en-1-yl]-1,3-benzothiazoles were synthesized from the reactions of 7-benzylidenebicyclo[3.2.0]hept-2-en-6-ones with 2-aminobenzenethiol. The antiproliferative activities of 2-[2-(2-phenylethenyl)cyclopent-3-en-1-yl]-1,3-benzothiazoles were determined against C6 (rat brain tumor) and HeLa (human cervical carcinoma cells) cell lines using BrdU cell proliferation ELISA assay. Cisplatin and 5-fluorouracil (5-FU) were used as standards. The most active compound was 2-{(1S,2S)-2-[(E)-2-(4-methylphenyl)ethenyl]cyclopent-3-en-1-yl}-1,3-benzothiazole against C6 cell lines with IC50=5.89 mu m value (cisplatin, IC50=14.46 mu m and 5-FU, IC50=76.74 mu m). Furthermore, the most active compound was 2-{(1S,2S)-2-[(E)-2-(2-methoxyphenyl)ethenyl]cyclopent-3-en-1-yl}-1,3-benzothiazole against HeLa cell lines with IC50=3.98 mu m (cisplatin, IC50=37.95 mu m and 5-FU, IC50=46.32 mu m). Additionally, computational studies of related molecules were performed by using B3LYP/6-31G+(d,p) level in the gas phase. Experimental IR and NMR data were compared with the calculated results and were found to be compatible with each other. Molecular electrostatic potential (MEP) maps of the most active 2-{(1S,2S)-2-[(E)-2-(2-methoxyphenyl)ethenyl]cyclopent-3-en-1-yl}-1,3-benzothiazole against HeLa and the most active 2-{(1S,2S)-2-[(E)-2-(4-methylphenyl)ethenyl]cyclopent-3-en-1-yl}-1,3-benzothiazole against C6 were investigated, aiming to determine the region that the molecule is biologically active. Biological activities of mentioned molecules were investigated with molecular docking analyses. The appropriate target protein (PDB codes: 1 M17 for the HeLa cells and 1JQH for the C6 cells) was used for 2-{(1S,2S)-2-[(E)-2-(2-methoxyphenyl)ethenyl]cyclopent-3-en-1-yl}-1,3-benzothiazole and 2-{(1S,2S)-2-[(E)-2-(4-methylphenyl)ethenyl]cyclopent-3-en-1-yl}-1,3-benzothiazole molecules exhibiting the highest biological activity against HeLa and C6 cells in the docking studies. As a result, it was determined that these molecules are the best candidates for the anticancer drug.
Evaluation of acetylcholinesterase and carbonic anhydrase inhibition profiles of 1,2,3,4,6-pentasubstituted-4-hydroxy-cyclohexanes
(WILEY, 2017) Kocyigit, Umit M.; Taslimi, Parham; Gezegen, Hayreddin; Gulcin, Ilhami; Ceylan, Mustafa
Carbonic anhydrase (CA; EC 4.2.1.1) is used for remedial purposes for several years, as there is significant focus on expanding more new activators (CAAs) and high affinity inhibitors. Alzheimers disease and other similar ailments such as dementia and vascular dementia with Lewy bodies reduce cholinergic activity in the important areas involved in cognition and memory. Prevalent drugs for the symptomatic therapy of dementia are significant in increasing the associated cholinergic deficiency by inhibiting acetylcholinesterase (AChE). These six-membered carbocycles showed nice inhibitory action against AChE and human carbonic anhydrase (hCA) II and I isoforms. The hCA I, II, and AChE were efficiently inhibited by these molecules, with K-i values in the range of 6.70-35.85nM for hCA I, 18.77-60.84nM for hCA II, and 0.74-4.60 for AChE, respectively.
Fenilüre Birimi İçeren 2-Benzoilindan-1-on ve İndenopirazol Türevlerinin Sentezi ve Antikanser Aktivitelerinin İncelenmesi
(2016) Gezegen, Hayreddin; Ceylan, Mustafa
Hetero halkalı bileşikler arasında yer alan pirazol türevlerinin biyoaktif bileşikler olduğu bilinmektedir. Pirazol sınıfının bir üyesi olan indenopirazol türevleri de biyoaktif potansiyeli yüksek bileşiklerdir. Bu çalışmada fenilüre birimi içeren yeni 1,3-diketon bileşiklerinin sentezi ve bu bileşikler üzerinden de yeni indenopirazol türevlerinin sentezi amaçlanmıştır. Elde edilen bu yeni bileşiklerin antikanser aktivitelerinin incelenmesi de hedefler arasındadır. Çalışmada öncelikle, 4?-aminoasetofenonun farklı sübstitüentlere sahip fenilizosiyanatlar ile reaksiyonundan fenilüre birimi içeren asetofenon türevleri (1a-j) elde edildi. Elde edilen asetofenon türevlerinin (1a-j) ftaldialdehit ile reaksiyonundan ise 2-benzoilindan-1-on türevleri (2a-j) sentezlendi. Sonrasında ise 2-benzoilindan-1-on türevlerinin (2a-j) hidrazin veya fenil hidrazin ile muamele edilmesinden fenilüre birimi içeren indenopirazol türevlerinin sentezi (3a- j ve 4a-j) yüksek verimlerle gerçekleştirildi. Elde edilen bileşiklerin karakterizasyonu spektroskopik yöntemler (1H-NMR, 13C-NMR, 2D-NMR, IR ve HPLC-TOF/MS) ile yapıldı. Son aşamada sentezlenen bileşiklerin antikanser aktiviteleri incelendi. Bileşiklerin HeLa (insan servikal kanser hücre hattı) ve C6 (sıçan beyin tümörü) hücre hatlarına karşı % 50 inhibisyon konsantrasyonları (IC50) ve gösterdikleri antiproliferatif etkiler yapılan deneyler ile belirlendi. Yapılan testler sonucunda sentezlenen bileşikler içerisinde hidrazinden elde edilen indenopirazol türevlerinin (3a-j) daha yüksek antikanser aktivitelere sahip oldukları görüldü. Daha sonra antiproliferatif etkileri yüksek bileşiklerin hücre döngüsünde ve apoptosiste rol oynayan temel genlerin ekspresyonu üzerine etkisi belirlendi. Bu bileşikler içerisinden 3b ve 3d bileşiklerinin yüksek derecede apoptotik özelliğe sahip oldukları belirlenmiştir.
Novel Aminothiazole-Chalcone Analogs: Synthesis, Evaluation Acetylcholinesterase Activity, In Silico Analysis
(Wiley-V C H Verlag Gmbh, 2025) Sarikaya, Meryem Kececi; Yildirim, Suheda; Kocyigit, Umit M.; Ceylan, Mustafa; Yirtici, Umit; Eyupoglu, Volkan
In this study, novel thiazole-chalcone analogs were synthesized, and their inhibitory effects on acetylcholinesterase (AChE) were examined. In vitro enzyme activity studies were conducted to calculate IC50 values, which were found to range between 2.55 and 72.78 mu M (tacrine IC50 = 53.31 mu M). The Ki values of the compounds showing the best inhibition (6g and 6e) were calculated and compared to those of the standard substance tacrine. All compounds reduced the AChE activity. Additionally, predictions made with SwissADME indicated that all compounds complied with Lipinski's rules and possessed good oral bioavailability properties, and the inhibitory effects of compounds 6e and 6g on AChE were evaluated using molecular docking and molecular dynamics simulations (100 ns). The results showed that compounds 6e and 6g had strong and stable interactions with AChE.
Potassium carbonate mediated one-pot synthesis and antimicrobial activities of 2-alkoxy-4-(aryl)-5H-indeno[1,2b] pyridine-3-carbonitriles
(ACG PUBLICATIONS, 2016) Ozturk, Sahin; Gurdere, Meliha Burcu; Gezegen, Hayreddin; Ceylan, Mustafa; Budak, Yakup
2-Alkoxy-4-(aryl)-5H-indeno[ 1,2-b] pyridine-3-carbonitriles (3a-e and 4a-e) were synthesized via multicomponent reaction from 2-aryl-methylidineindan-1-ones (1a-e), malononitrile and K2CO3 in ethanol and/or methanol. The structures of obtained compounds (3a-e and 4a-e) were characterized using the spectroscopic methods (NMR, IR) and elemental analysis. Addition, the in vitro antimicrobial activities of compounds (3a-e) were tested against the five human pathogenic bacteria. Penicillin G and Ceftriaxone antibiotics were used as positive control. The results were given as MIC values (minimum inhibition concentration), and compounds 3b-d showed very high activity against Escherichia coli 111.
Purification of glutathione S-transferase enzyme from quail liver tissue and inhibition effects of (3aR,4S,7R,7aS)-2-(4-((E)-3-(aryl)acryloyl)phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives on the enzyme activity
(WILEY, 2018) Temel, Yusuf; Kocyigit, Umit M.; Taysi, M. Serif; Gokalp, Faik; Gurdere, Meliha Burcu; Budak, Yakup; Ceylan, Mustafa; Gulcin, Ilhami; Ciftci, Mehmet
The use of quail meat and eggs has made this animal important in recent years, with its low cost and high yields. Glutathione S-transferases (GST, E.C.2.5.1.18) are an important enzyme family, which play a critical role in detoxification system. In our study, GST was purified from quail liver tissue with 47.88-fold purification and 12.33% recovery by glutathione agarose affinity chromatography. The purity of enzyme was checked by SDS-PAGE method and showed a single band. In addition, inhibition effects of (3aR,4S,7R,7aS)-2-(4-((E)-3-(aryl)acryloyl)phenyl)-3a,4,7,7a-tetrahydro-1H-4,7methanoisoindole-1,3(2H)-dion derivatives (1a-g) were investigated on the enzyme activity. The inhibition parameters (IC50 and K-i values) were calculated for these compounds. IC50 values of these derivatives (1a-e) were found as 23.00, 15.75, 115.50, 10.00, and 28.75M, respectively. K-i values of these derivatives (1a-e) were calculated in the range of 3.04 +/- 0.50 to 131.50 +/- 32.50M. However, for f and g compounds, the inhibition effects on the enzyme were not found.
Some old 2-(4-(Aryl)- thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7- tethanoisoindole-1,3(2H)-dione derivatives: Synthesis, inhibition effects and molecular docking studies on Aldose reductase and ?-Glycosidase
(2021) Taslimi, Parham; Demir, Yeliz; Duran, Hatice Esra; Koçyiğit, Ü.Muhammet; Tuzun, Burak; Aslan, Osman Nuri; Ceylan, Mustafa
Utilizing the simple chromatic techniques, Aldose reductase (AR) was derived from sheep liver. In addition, ?-glycosidase from Saccharomyces cerevisiae was used as the enzyme. It was determined the interactions between compounds and the enzymes. Molecular docking method used to compare biological activity values of molecules against enzymes. In the current study, the inhibition effect of synthetic isoindol-substitute thiazole derivatives (3a-f) on AR, and ?-glycosidase enzymes was studied. In the thiazole series, compound 3b (Ki: 9.70±4.72 ?M) showed a maximum inhibitory impact towards AR while compound 3f (Ki: 44.40±17.18 ?M) showed a lowest inhibitory impact towards AR. It was investigated potent inhibition profiles with Ki values in the range of 24.54±6.92–44.25±10.34 ?M against ?-glycosidase. Theoretical results were found consistent with experimental results. Acting as antidiabetic agents, these compounds have the potential to be the selective inhibitor of ?-glycosidase and AR enzymes. The biological activities of the studied molecules against AR and ?-glycosidase enzymes will be compared with molecular docking method. ADME analysis of the molecules will be done.
Some old 2-(4-(Aryl)- thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-tethanoisoindole-1,3(2H)-dione derivatives: Synthesis, inhibition effects and molecular docking studies on Aldose reductase and α-Glycosidase
(Sivas Cumhuriyet Üniversitesi, 2021) Taslımı, Parham; Demir, Yeliz; Duran, Hatice Esra; Koçyiğit, Ümit Muhammet; Tüzün, Burak; Aslan, Osman Nuri; Ceylan, Mustafa
Utilizing the simple chromatic techniques, Aldose reductase (AR) was derived from sheep liver. In addition, α-glycosidase from Saccharomyces cerevisiae was used as the enzyme. It was determined the interactions between compounds and the enzymes. Molecular docking method used to compare biological activity values of molecules against enzymes.In the current study, the inhibition effect of synthetic isoindol-substitute thiazole derivatives (3a-f) on AR, and α-glycosidase enzymes was studied. In the thiazole series, compound 3b (Ki: 9.70±4.72 M) showed a maximum inhibitory impact towards AR while compound 3f (Ki: 44.40±17.18 M) showed a lowest inhibitory impact towards AR. It was investigated potent inhibition profiles with Ki values in the range of 24.54±6.92–44.25±10.34 M against α-glycosidase. Theoretical results were found consistent with experimental results.Acting as antidiabetic agents, these compounds have the potential to be the selective inhibitor of α-glycosidase and AR enzymes. The biological activities of the studied molecules against AR and α-glycosidase enzymes will be compared with molecular docking method. ADME analysis of the molecules will be done.
Synthesis and Antimicrobial Activity of Racemic 1,5-Diols: 2-(1,3-Diaryl-3-hydroxypropyl)cyclohexan-1-ol Derivatives
(WILEY-V C H VERLAG GMBH, 2016) Gezegen, Hayreddin; Tutar, Ugur; Ceylan, Mustafa
A series of novel racemic 2-(1,3-diaryl-3-hydroxypropyl)cyclohexan-1-ol derivatives were synthesized from 1,5-diketones. All the synthesized compounds were characterized by spectroscopic methods. The antibacterial activities of obtained chiral 1,5-diols were investigated against four Gram-positive and three Gram-negative bacteria by determining of minimum inhibitory concentrations (MICs) in vitro. Compounds 3b, 3c, and 3d were found to be active against Enterococcus faecalis and Escherichia coli. In addition, compound 3j were found to be moderately active against all tested bacterial strains.
Synthesis and Biological Evaluation of Novel 1-(4-(Hydroxy(1-oxo-1,3-dihydro-2H-inden-2-ylidene)methyl)phenyl)-3-phenylurea Derivatives
(WILEY-V C H VERLAG GMBH, 2017) Gezegen, Hayreddin; Hepokur, Ceylan; Tutar, Ugur; Ceylan, Mustafa
A series of novel phenylurea containing 2-benzoylindan-1-one derivatives 3a - 3j were synthesized from the reaction of phenylurea-substituted acetophenones 1a - 1j with phthalaldehyde 2 under mild reaction conditions in good yields. All synthesized compounds were characterized by spectroscopic methods. The obtained compounds (3a - 3j) were evaluated for anticancer activity against HeLa and C6 cell lines. Antiproliferative activity was determined by the BrdU proliferation ELISA assay, 3f and 3g were found to be most active compounds. The compounds were also screened for antimicrobial activity and all compounds showed remarkable activity against used microorganisms.
Synthesis and biological evaluation of novel indenopyrazole derivatives
(WILEY, 2019) Gezegen, Hayreddin; Tutar, Ugur; Hepokur, Ceylan; Ceylan, Mustafa
A series of novel indenopyrazole derivatives 2a-j and 3a-j were synthesized from the reaction of 1-(4-(hydroxy(1-oxo-1,3-dihydro-2H-inden-2-ylidene)methyl)phenyl)-3-phenylurea derivatives 1a-j with hydrazine and phenylhydrazine, respectively. The obtained novel indenopyrazoles (2a-j and 3a-j) were evaluated for anticancer activity against HeLa and C6 cell lines. Antiproliferative activity was determined by the BrdU proliferation ELISA assay; 2a, 2b, 2d, 2h, and 3h were found to be the most active compounds. The compounds were also screened for antimicrobial activity, and all compounds showed moderate activity against used microorganisms.
Synthesis and Carbonic Anhydrase Inhibition of Novel 2-(4-(Aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione Derivatives
(WILEY-V C H VERLAG GMBH, 2016) Kocyigit, Umit M.; Aslan, Osman Nuri; Gulcin, Ilhami; Temel, Yusuf; Ceylan, Mustafa
Carbonic anhydrase (CA, EC 4.2.1.1) is a member of the metalloenzyme family. It catalyzes the rapid conversion of carbon dioxide (CO2) and water to bicarbonate (HCO3-) and protons (H+) and also plays an important role in biochemical and physiological processes. In this study, a number of novel 2-(4-(aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives were synthesized and evaluated for their inhibitory characteristics against the human CA isoenzymes I and II (hCA I and hCA II). The structures of the new molecules 8a-i were confirmed by means of IR, H-1 NMR, C-13 NMR, and elemental analysis. These compounds exhibited excellent inhibitory effects, in the low nanomolar range, with K-i values in the range of 27.07-37.80 nM against hCA I and in the range of 11.80-25.81nM against hCA II. Our findings suggest that the new isoindolylthiazole derivatives have superior inhibitory effect over acetazolamide (AZA), which is used as clinical CA inhibitor with K-i values of 34.50 and 28.93nM against the hCA I and hCA II isoenzymes, respectively.
Synthesis and Carbonic Anhydrase Inhibition of Tetrabromo Chalcone Derivatives
(WILEY-V C H VERLAG GMBH, 2017) Kocyigit, Umit M.; Budak, Yakup; Eliguzel, Fikret; Taslimi, Parham; Kilic, Deryanur; Gulcin, Ilhami; Ceylan, Mustafa
In the present study, human carbonic anhydrase (hCA) enzyme was purified and characterized from fresh blood human red cells by Sepharose-4B-l-tyrosine-sulfanilamide affinity gel chromatography. Secondly, a series of new tetrabromo chalcone derivatives containing 4,7-methanoisoindol-1,3-dione (2a-i) were synthesized from the addition of Br-2 to related chalcone derivatives (1a-i). The structures of the new molecules (2a-i) were confirmed by means of H-1 NMR, C-13 NMR and elemental analysis. Finally, the inhibitory effects of 2a-i on CA activities were investigated using the esterase method under in vitro conditions. The compounds 2a-i exhibited excellent inhibitory effects, in the low nanomolar range, with K-i values in the range of 11.30-21.22nM against hCA I and in the range of 8.21-12.86nM against hCA II. Our findings suggest that the new compounds 2a-i have superior inhibitory effect over acetazolamide (AZA), which is used as clinical CA inhibitor, with obtained K-i values of 34.50 and 28.93nM against the hCA I and II isozymes, respectively. In addition to the inhibition assays, molecular modeling approaches were implemented for prediction of the binding affinities of compounds 2a and 2c, which had the highest inhibition effects, against the hCA I and II isozymes.
Synthesis and investigation of antibacterial activities and carbonic anhydrase and acetyl cholinesterase inhibition profiles of novel 4,5-dihydropyrazol and pyrazolyl-thiazole derivatives containing methanoisoindol-1,3-dion unit
(TAYLOR & FRANCIS INC, 2017) Budak, Yakup; Kocyigit, Umit M.; Gurdere, Meliha Burcu; Ozcan, Kezban; Taslimi, Parham; Gulcin, Ilhami; Ceylan, Mustafa
Novel 4,5-dihydropyrazole derivatives (3a-i), 3-(4-((3aR,4S,7R,7aS)-1,3-dioxo-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindol-2(3H)-yl)phenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothio amide, were obtained by the addition of thiosemicarbazide (2) to the chalcones (1a-i). The addition-cyclization of 2,4-dibromoacetophenone (4) to pyrazole derivatives (3a-i) gave the new pyrazolyl-thiazole derivatives (5a-i), (3aR,4S,7R,7aS)-2-(4-(1-(4-(4-bromophenyl)thiazol-2-yl)-5-phenyl-4,5-dihydro-1H-pyrazol-3-yl)phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione. Antibacterial and acetylcholinesterase (AChE) enzyme and human carbonic anhydrase (hCA) I, and II isoform inhibitory activities of the compounds 3a-i and 5a-i were investigated. Some of the compounds showed promising antibacterial activity. In addition, the hCA II and I were effectively inhibited by the lately synthesized derivatives, with K-i values in the range of 18.90 +/- 2.37 -58.25 +/- 13.62nM for hCA II and 5.72 +/- 0.98 -37.67 +/- 5.54nM for hCA I. Also, the K-i parameters of these compounds for AChE were obtained in the range of 25.47 +/- 11.11-255.74 +/- 82.20nM. Also, acetazolamide, clinical molecule, was used as a CA standard inhibitor that showed K-i value of 70.55 +/- 12.30nM against hCA II, and 67.17 +/- 9.1nM against hCA I, and tacrine inhibited AChE showed K-i value of 263.67 +/- 91.95. [GRAPHICS] .
Synthesis and investigation of anticancer, antibacterial activities and carbonic anhydrase, acetylcholinesterase inhibition profiles of novel (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones
(SPRINGER WIEN, 2019) Kocyigit, Umit M.; Budak, Yakup; Gurdere, Meliha Burcu; Duru, Nese; Taslimi, Parham; Gulcin, Ilhami; Ceylan, Mustafa
A series of novel 1,3,5-trisubstituted pyrazoline derivatives, (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones, were synthesized and evaluated for their antimicrobial and anticancer activities. In addition, the compounds were tested against acetylcholinesterase (AChE) enzyme and two physiologically relevant carbonic anhydrase I and II isozymes (hCA I and II). In this study, inhibition of hCA I and hCA II by the novel synthesized 1,3,5-trisubstituted pyrazolines was impressive, with K-i values in the range of 3.33-7.90nM for hCA I and 2.07-8.47nM for hCA II, while the K-i values of these compounds for AChE were recorded in the range of 9.61-48.42nM, respectively. Two compounds can be investigated as the leader compounds because of their lowest K-i values to make further detailed CA inhibition studies. [GRAPHICS] .
Synthesis of chalcone-imide derivatives and investigation of their anticancer and antimicrobial activities, carbonic anhydrase and acetylcholinesterase enzymes inhibition profiles
(TAYLOR & FRANCIS LTD, 2018) Kocyigit, Umit Muhammet; Budak, Yakup; Gurdere, Meliha Burcu; Erturk, Fatih; Yencilek, Belkiz; Taslimi, Parham; Gulcin, Ilhami; Ceylan, Mustafa
The new 1-(4-(3-(aryl)acryloyl)phenyl)-1H-pyrrole-2,5-diones (5a-g) were prepared from 4-aminchalcones (3a-g) and screened for biological activities. All compounds (3a-g and 5a-g), except 3d and 3e displayed good cytotoxic activities with IC50 values in the range of 7.06-67.46 mu M. IC50 value of 5-fluorouracil (5-FU) was 90.36 mu M. Moreover, most of compounds 5a-g showed high antibacterial activity with 8-20 mm of inhibition zone (19-25mm of Sulbactam-Cefoperazone (SCF)). In addition, they showed good inhibitory action against acetylcholinesterase (AChE), and human carbonic anhydrase I, and II (hCA I and hCA II) isoforms. Also, these compounds demonstrated effective inhibition profiles with Ki values of 426.47-699.58 nM against hCA I, 214.92-532.21 nM against hCA II, and 70.470-229.42nM against AChE. On the other hand, acetazolamide, clinically used drug, showed a Ki value of 977.77 +/- 227.4nM against CA I, and 904.47 +/- 106.3 nM against CA II, respectively. Also, tacrine inhibited AChE showed a Ki value of 446.56 +/- 58.33 nM.
Synthesis, carbonic anhydrase I and II isoenzymes inhibition properties, and antibacterial activities of novel tetralone-based 1,4-benzothiazepine derivatives
(WILEY, 2017) Ceylan, Mustafa; Kocyigit, Umit M.; Usta, Necibe Canan; Gurbuzlu, Belma; Temel, Yusuf; Alwasel, Saleh H.; Gulcin, Ilhami
Benzothiazepine compounds have a wide range of applications such as antibacterial, antidepressants, anticonvulsants, antihypertensives, antibiotics, antifungal, hypnotic, enzyme inhibitors, antitumor, anticancer and anti-HIV agents. In this study, the synthesis of novel tetralone-based benzothiazepine derivatives (1-16) and their in vitro antibacterial activity and human carbonic anhydrase isoenzymes I and II ( hCA I and II) inhibitory effects were investigated. Both isoenzymes were purified by sepharose-4B-L-tyrosine-sulfanilamide affinity chromatography from fresh human red blood cells. All compounds demonstrated the low nanomolar inhibitory effects on both isoenzymes using esterase activity. Benzothiazepine derivative 2 demonstrated the best hCA I inhibitory effect with Ki value of 18.19 nM. Also, benzothiazepine derivative 7 showed the best hCA II inhibitory effect with Ki value of 11.31 nM. On the other hand, acetazolamide clinically used as CA inhibitor, showed Ki value of 19.92 nM against hCA I and 33.60 nM against hCA II, respectively.
Synthesis, characterization, anticancer, antimicrobial and carbonic anhydrase inhibition profiles of novel (3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives
(ACADEMIC PRESS INC ELSEVIER SCIENCE, 2017) Kocyigit, Umit M.; Budak, Yakup; Gurdere, Meliha Burcu; Tekin, Saban; Koprulu, Tugba Kul; Erturk, Fatih; Ozcan, Kezban; Gulcin, Ilhami; Ceylan, Mustafa
In the present study, a series of new hybrid compounds containing chalcone and methanoisoindole units 7a-n ((3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl) acryloyl) phenyl)-3a, 4,7,7a-tetrahydro-1H-4,7-methanoisoin dole-1,3(2H)-dione) were synthesized, characterized and investigated for their anticancer activity against C6 gliocarcinoma cell in rats, and antimicrobial activity against some human pathogen microorganisms. The compounds 7e, 7h, 7j, 7k, 7L and 7n showed very high anticancer activity with the inhibition range of 80.51-97.02% compared to 5-FU. Some of the compounds exhibited anti-microbial activity. Also, they evaluated for inhibition effects against human carbonic anhydrase I, and II isoenzymes (hCA I and II) with Ki values in the range of 405.26-635.68 pM for hCA I, and 245.40-489.60 pM for hCA II, respectively. These results demonstrated that 3aR, 4S, 7R, 7aS)-2-(4-((E)-3-(3-aryl) acryloyl) phenyl)-3a, 4,7,7a-tetrahy dro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives could be used in different biomedical applications. (C) 2016 Elsevier Inc. All rights reserved.

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